Assay Detail
Binding
CHEMBL2168992
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Displacement of [3H]epibatidine from rat alpha2beta4 nACHR
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha2/beta4 (CHEMBL1907590) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.39 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165439 | — | — | 1 | 7.52 |
| CHEMBL2165452 | — | — | 1 | 7.24 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.16 |
| CHEMBL2165438 | — | — | 1 | 6.84 |
| CHEMBL2165440 | — | — | 1 | 6.79 |
| CHEMBL2165444 | — | — | 1 | 6.51 |
| CHEMBL2165453 | — | — | 1 | 6.50 |
| CHEMBL2165443 | — | — | 1 | 6.33 |
| CHEMBL2165445 | — | — | 1 | 5.24 |
| CHEMBL2165441 | — | — | 1 | 5.18 |
| CHEMBL2165442 | — | — | 1 | 5.00 |
| CHEMBL2165451 | — | — | 1 | - |
| CHEMBL2165450 | — | — | 1 | - |
| CHEMBL2165446 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165439 | — | Ki | = | 30.3 | nM | 7.52 |
| CHEMBL2165452 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3 | NICOTINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2165438 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL2165440 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL2165444 | — | Ki | = | 311.0 | nM | 6.51 |
| CHEMBL2165453 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2165443 | — | Ki | = | 472.0 | nM | 6.33 |
| CHEMBL2165445 | — | Ki | = | 5810.0 | nM | 5.24 |
| CHEMBL2165441 | — | Ki | = | 6570.0 | nM | 5.18 |
| CHEMBL2165442 | — | Ki | = | 9970.0 | nM | 5.00 |
| CHEMBL2165451 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2165450 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2165446 | — | Ki | > | 10000.0 | nM | - |